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丝素纳米粒:天然抗氧化剂槲皮素的有效载体。

Silk fibroin nanoparticles: Efficient vehicles for the natural antioxidant quercetin.

机构信息

Departmento de Biotecnología, Instituto Murciano de Investigación y Desarrollo Agrario y Alimentario (IMIDA), La Alberca, Murcia, 30150, Spain.

Departamento de Producción, Centro Nacional de Sanidad Agropecuaria (CENSA), San José de las Lajas (Mayabeque), 32700, Cuba.

出版信息

Int J Pharm. 2017 Feb 25;518(1-2):11-19. doi: 10.1016/j.ijpharm.2016.12.046. Epub 2016 Dec 21.

Abstract

This article describes how silk fibroin nanoparticles (SFNs) are capable of adsorbing and releasing quercetin (Q) and how its integrity is highly preserved, as confirmed by antioxidant activity assays. Q loading onto SFNs was optimized in terms of the Q/SFN ratio (w/w), time of adsorption and solvent mixture. Quercetin-loaded silk fibroin nanoparticles (QSFNs) were characterized using the dynamic light scattering technique to measure the diameter (Z-Average) and Z-potential (ζ). Loaded particles were slightly bigger than the SFNs, while their ζ was less negative. The antioxidant activity against DPPH showed that the Q loaded in QSFNs not only retains the antioxidant activity but also has a synergistic scavenging activity due the intrinsic antioxidant activity of the SF. The drug loading content (DLC) and the encapsulation efficiency (EE) varied with the relation between Q and SFN in the loading solution. The sustained release of Q occurred throughout the experiment both in phosphate buffer saline (pH 7.4) and simulated intestinal fluid (pH 6.8). The results point to SFNs as promising candidates for Q loading, transport and gastrointestinal delivery with potential applications in nanomedicine, while retaining their nano-size and their antioxidant properties.

摘要

本文描述了丝素纳米粒子(SFNs)如何能够吸附和释放槲皮素(Q),以及其完整性如何得到高度保护,这一点通过抗氧化活性测定得到了证实。通过 Q/SFN 比例(w/w)、吸附时间和溶剂混合物对 Q 加载到 SFNs 进行了优化。使用动态光散射技术对载有 Q 的丝素纳米粒子(QSFNs)进行了表征,以测量直径(Z-平均)和 Z 电位(ζ)。负载的粒子比 SFNs 略大,而其 ζ 则不那么负。对 DPPH 的抗氧化活性表明,载于 QSFNs 中的 Q 不仅保留了抗氧化活性,而且由于 SF 的固有抗氧化活性还具有协同清除活性。药物载量(DLC)和包封效率(EE)随载药溶液中 Q 与 SFN 的关系而变化。在磷酸盐缓冲盐水(pH7.4)和模拟肠液(pH6.8)中,Q 均发生持续释放。研究结果表明 SFNs 有望成为 Q 负载、运输和胃肠道给药的候选材料,具有纳米医学的潜在应用,同时保持其纳米尺寸和抗氧化特性。

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